Construction of key building blocks towards the synthesis of cortistatins,Organic & Biomolecular Chemistry

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Construction of key building blocks towards the synthesis of cortistatins
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020/03/02 , DOI: 10.1039/d0ob00170h
Satrajit Indu _{1,

2,

3,

4} , Rahul D. Telore _{1,

2,

3,

4} , Krishna P. Kaliappan _{1,

2,

3,

4}

Affiliation

This work reports the construction of key building blocks towards the synthesis of cortistatins; a family of steroidal alkaloids. Cortistatin A, being a primary target due to its superior biological properties over other congeners, has been prepared by two different synthetic routes. Synthesis of the precursor to the heavily substituted A-ring starting from D-glucose and construction of the DE-ring junction employing a Hajos–Parrish ketone as a chiral pool have been demonstrated. Efforts are underway to assemble these key fragments and build towards the total synthesis of cortistatin A.

中文翻译：

构建皮质醇合成的关键组成部分

这项工作报告了合成皮质抑素的关键组成部分的构建；甾体生物碱家族。Cortistatin A由于具有比其他同类产品优越的生物学特性而成为主要靶标，已通过两种不同的合成途径制备。已经证明了从D-葡萄糖开始合成重取代的A环的前体，以及使用Hajos-Parrish酮作为手性库的DE环连接结构。正在努力组装这些关键片段，并逐步实现皮质抑素A的全合成。

更新日期：2020-04-01

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